Estrone C15 derivatives--a new class of 17beta-hydroxysteroid dehydrogenase type 1 inhibitors

JOSEF MESSINGER, Messinger J, Bettina Husen, Husen B, Koskimies P, Pasi Koskimies, Leena Hirvelä, Hirvelä L, Lila Kallio, Kallio L, Pauli Saarenketo, Saarenketo P, Hubert Thole, Thole H
Molecular and cellular endocrinology · 2009 · doi:10.1016/j.mce.2008.10.022 · PMID:19014997
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Researchers designed estrone C15 derivatives as potential treatments for endometriosis and identified compound 21 as a potent, selective 17beta-HSD1 inhibitor lacking estrogenic activity.

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The provided text does not contain a scientific paper but rather a security challenge page generated by the Anubis anti-scraping system. It explains that the website is protected against automated bots using a Proof-of-Work scheme similar to Hashcash to mitigate server load from mass scrapers. The message instructs users to enable modern JavaScript features and disable privacy plugins like JShelter to access the content. This paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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Abstract

Lowering local estradiol concentration by inhibition of the estradiol-synthesizing enzyme 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) has been proposed as a promising new therapeutic option to treat estrogen-dependent diseases like endometriosis and breast cancer. Based on a molecular modelling approach we designed and synthesized novel C15-substituted estrone derivatives. Subsequent biological evaluation revealed that potent inhibitors of human 17beta-HSD1 can be identified in this compound class. The best, compound 21, inhibited recombinant human 17beta-HSD1 with an IC50 of 10nM and had no effect on the activity of recombinant human 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2), the enzyme catalyzing estradiol inactivation. These properties were retained in a cell-based enzyme activity assays. In spite of the estrogen backbone compound 21 did not show estrogen receptor mediated effects in vitro or in vivo. In conclusion, estrone C15 derivative compound 21 can be regarded as a promising lead compound for further development as a 17beta-HSD1 inhibitor.
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Condition tags

endometriosis

MeSH descriptors

Enzyme Inhibitors Estradiol Dehydrogenases Estrone Estrone Animals Binding Sites Crystallography, X-Ray Enzyme Inhibitors Enzyme Inhibitors Enzyme Inhibitors Estradiol Estradiol Estradiol Dehydrogenases Estrone Estrone Humans Models, Molecular

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europepmc
last seen: 2026-10-04T09:26:46.659050+00:00
pubmed
last seen: 2026-05-13T22:14:24.299271+00:00
unpaywall
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